a Department of Pharmaceutical Engineering & Technology Indian Institute of Technology (BHU) , Varanasi , India.
Artif Cells Nanomed Biotechnol. 2018;46(sup3):S546-S555. doi: 10.1080/21691401.2018.1501379. Epub 2018 Oct 16.
Quercetin (Qu), is a flavonoid known to have anti-diabetic effects owing to its antioxidant property, thus promoting regeneration of the pancreatic islets, ultimately increasing insulin secretion. But the therapeutic application of Qu is hampered by its low oral bioavailability and its unfavourable physicochemical characteristics. The present work aimed at formulation of Quercetin loaded Soluplus® micelles (SMs) so as to enhance its bioavailability and provide prolonged release for the management of diabetes. Box-Behnken response surface methodology was employed to optimize the formulation prepared using co-solvent evaporation method. Physicochemical characterization confirmed the nano-spherical nature of Quercetin loaded Soluplus® micelles (Qu-SMs) with average particle size ranging from 85-108nm, encapsulation efficiency of 63-77%. Solid state characterization confirmed the encapsulation of Qu in the micelles without any incompatibilities. Moving forward, the results of in vitro study revealed prolonged and slow release of Qu from the developed formulations. The in vivo pharmacokinetic study revealed improved bioavailability by enveloping the drug in SMs. Moreover, the study performed to evaluate the efficiency in diabetes treatment revealed an enhanced anti-diabetic effect. Thus, Qu-SMs can serve as potential carriers aimed at improving the anti-diabetic property of Qu.
槲皮素(Qu)是一种具有抗氧化特性的黄酮类化合物,已知具有抗糖尿病作用,因此促进胰岛的再生,最终增加胰岛素的分泌。但是,由于其低口服生物利用度和不良的物理化学特性,Qu 的治疗应用受到了阻碍。本工作旨在通过将槲皮素负载于 Soluplus®胶束(SMs)中来提高其生物利用度并提供延长释放,从而管理糖尿病。采用 Box-Behnken 响应面法来优化使用共溶剂蒸发法制备的制剂。物理化学特性分析证实了 Qu 负载 Soluplus®胶束(Qu-SMs)具有纳米球性质,平均粒径为 85-108nm,包封效率为 63-77%。固态特性分析证实了 Qu 被包裹在胶束中,没有任何不相容性。接下来,体外研究结果表明,从开发的制剂中可以延长和缓慢释放 Qu。体内药代动力学研究表明,将药物包裹在 SMs 中可以提高生物利用度。此外,进行的评估糖尿病治疗效率的研究表明,增强了抗糖尿病作用。因此,Qu-SMs 可以作为潜在的载体,旨在提高 Qu 的抗糖尿病特性。